Sindopa
Sindopa: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Syndopa
ATX code: N04BA02
Active ingredient: levodopa (levodopa), carbidopa (carbidopa)
Producer: Sun Pharmaceutical Industries, Ltd. (India)
Description and photo update: 2018-21-11
Prices in pharmacies: from 183 rubles.
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Sindopa is an antiparkinsonian drug.
Release form and composition
Sindopa dosage form - tablets:
- dosage 250 + 25 mg: light pink, interspersed, flat-cylindrical, round with two intersecting risks and a chamfer on one and Syndopa engraving on the other side (10 pcs in strips, 5 strips in a cardboard box);
- dosage 100 + 10 mg: appearance is not described (in contoured packs without cells, 10 pcs., in a carton box 5 packs).
Composition of 1 tablet at a dosage of 250 + 25 mg:
- active substances: levodopa - 250 mg; carbidopa - 25 mg;
- auxiliary components: corn starch (dried) - 5 mg; sodium carboxymethyl starch (type A) - 20 mg; colloidal silicon dioxide - 2 mg; magnesium stearate - 5 mg; talc - 10 mg; butylhydroxyanisole - 0.01 mg; povidone-K30 - 12 mg; crimson dye (Ponso 4R) - 0.3 mg; microcrystalline cellulose - 50 mg; corn starch - 48.848 mg; lactose - 95 mg.
Composition of 1 tablet at a dosage of 100 + 10 mg: active ingredients: levodopa - 100 mg; carbidopa - 10 mg; there is no data on the composition of auxiliary components.
Pharmacological properties
Pharmacodynamics
Levodopa is an amino acid derived from L-tyrosine. With the participation of a cytoplasmic enzyme (aromatic L-amino acids, decarboxylase), dopamine is formed directly from levodopa. The end result of the effects of dopamine is the suppression of neuronal activity in the striatum of the brain. In peripheral tissues, under the influence of pyridoxine-dependent decarboxylase of aromatic amino acids, levodopa is rapidly decarboxylated, turning into dopamine, which, however, does not penetrate the blood-brain barrier.
The process of decarboxylation of levodopa in peripheral tissues inhibits carbidopa, which does not penetrate the blood-brain barrier and does not affect the conversion of levodopa to dopamine in the central nervous system. Thus, the use of a combination of levodopa with carbidopa can increase the amount of levodopa entering the brain. The bioavailability of levodopa when taken orally with carbidopa is doubled. Carbidopa never causes complete inhibition of aromatic L-amino acid decarboxylase.
Pharmacokinetics
Characteristic of carbidopa:
- absorption: C max (maximum concentration in blood plasma) after oral administration in a single dose in Parkinson's disease varies from 1.5 to 5 hours;
- metabolism and excretion: metabolized in the liver; the main metabolites excreted in the urine are alpha-methyl-3.4-dihydroxyphenylpropionic and alpha-methyl-3-methoxy-4-hydroxyphenylpropionic acid, which, respectively, make up 10 and 14% of metabolites excreted by the kidneys; in smaller quantities, 3.4-dihydroxyphenyl-acetone and N-methyl-carbidopa are found, their content is 5% (no more) of the total amount of metabolites; unchanged carbidopa is also found in the urine; conjugates have not been identified; excretion in the urine of carbidopa in unchanged form is mainly completed within 7 hours and is 35%.
Characteristics of levodopa:
- absorption: rapidly absorbed from the gastrointestinal tract and actively metabolized; forms more than 30 different metabolites, mainly converted to norepinephrine, epinephrine and dopamine; The max of a single dose of levodopa after oral administration in patients with Parkinson's disease varies from 1.5 to 2 hours, and is kept at a therapeutic level for 4–6 hours;
- excretion: levodopa metabolites are rapidly excreted in the urine - about ⅓ of the dose is excreted within 2 hours; T 1/2 (half-life) is approximately 50 minutes and rises to almost 1.5 hours when combined with carbidopa.
Effect of carbidopa on levodopa metabolism:
- an increase in the concentration of levodopa in blood plasma by 5 times with the previous intake of carbidopa;
- increasing the time to maintain the therapeutic concentration of levodopa in plasma from 4 to 8 hours;
- increased T 1/2 of levodopa from 3 to 15 hours when taken in patients with Parkinson's disease in a single dose, previously treated with carbidopa;
- an increase in the concentration of levodopa by 3 times (at least) due to carbidopa;
- a decrease in the concentration of homovanilic acid and dopamine in urine and blood plasma with the preliminary intake of carbidopa.
Indications for use
According to the instructions, Sindopa is prescribed for the treatment of a disease or Parkinson's syndrome of a known origin: due to intoxication with toxic substances (including carbon monoxide or manganese), cerebrovascular disorders, encephalitis.
Contraindications
Absolute:
- melanoma or suspicion of it;
- skin pathologies of unknown nature;
- Huntington's disease;
- essential tremor;
- severe psychosis or neurosis;
- angle-closure glaucoma;
- glucose-galactose malabsorption, lactose intolerance, lactase deficiency;
- secondary parkinsonism caused by taking antipsychotics;
- combined treatment with non-selective monoamine oxidase (MAO) inhibitors, a period of 14 days after their intake;
- pregnancy and lactation;
- age under 18;
- individual intolerance to the components contained in the preparation.
Relative (diseases / conditions in the presence of which the appointment of Sindopa requires caution):
- severe violations of liver and kidney function;
- erosive and ulcerative lesions of the stomach and / or duodenum;
- heart failure;
- myocardial infarction with a history of heart rhythm disturbances;
- severe lung pathologies, including bronchial asthma;
- endocrine system diseases, including diabetes mellitus;
- severe psychosis and neurotic disorders;
- a history of epileptic seizures.
Instructions for use of Sindopa: method and dosage
Sindop tablets are taken orally, do not chew, with a small amount of food or after a meal with water.
Since there is competition between levodopa and aromatic amino acids for absorption, it is important to avoid consuming large amounts of protein while taking the drug. On average, the daily dose of carbidopa required to suppress the peripheral conversion of levodopa varies from 0.07 to 0.1 g. Exceeding 0.2 g of carbidopa does not entail further enhancement of the therapeutic effect. The maximum daily dose of levodopa is no more than 2 g.
The initial dose of Sindopa (tablets of 0.25 + 0.025 g) is ½ pcs. 2 times a day, with a possible increase, if necessary, by ½ pcs. per day or every other day until the optimal effect is achieved. On the first day, and sometimes even after taking the first dose, a therapeutic effect appears. Full clinical effect is observed after 7 days of drug intake. Usually, at the beginning of replacement treatment, the daily dose should not exceed 3 pcs. per day (1 pc. 3 times a day). The appointment of this dosage is recommended at the beginning of therapy for severe cases of the disease. As an exception, with monotherapy, the daily dose can be increased, but not more than 8 pcs. (1 piece 8 times a day). Take more than 6 pieces with great care. per day.
In cases of switching from levodopa drugs, they stop taking them at least 12 hours before the start of Sindopa therapy; when switching from prolonged forms - in 24 hours. The daily dose of the drug should provide approximately 20% of the previous daily dose of levodopa.
The initial dose of Sindopa for patients who received more than 1.5 g of levodopa is 1 pc. 3-4 times a day.
Side effects
- nervous system: dementia, increased libido, hypomania, depression with or without suicidal intentions, hallucinations, changes in mental status (including transient psychoses and paranoid effects), insomnia, anxiety, increased anxiety, headache, nervous tension, nightmares, confusion consciousness, drowsiness, sedation, convulsions, dystonic involuntary movements, dizziness, neuroleptic malignant syndrome, dystonia, dyskinesia (including choreoathetosis); with prolonged use - on-off syndrome;
- digestive system: anorexia, nausea, vomiting, constipation, diarrhea, epigastric pain, dry mouth, darkening of saliva, ulcerogenic effect in predisposed patients, gastrointestinal bleeding;
- cardiovascular system: phlebitis, increased blood pressure, tachycardia, arrhythmias, collapse, orthostatic hypotension;
- hematopoietic organs: agranulocytosis, thrombocytopenia, anemia (including hemolytic), leukopenia;
- respiratory system: upper respiratory tract infections, shortness of breath;
- urinary system: dark urine, frequent urination, urinary tract infections;
- allergic reactions: Shenlein-Genoch disease, skin rash, itching, urticaria, angioedema;
- laboratory parameters: positive direct Coombs' test; hypercreatinemia; hyperuricemia; change in the concentration of urea nitrogen, bilirubin and iodine associated with protein; changes in the activity of lactate dehydrogenase, alkaline phosphatase, aspartate aminotransferase, alanine aminotransferase;
- others: chest pain, fainting.
Possible side effects of levodopa to consider when prescribing levodopa + carbidopa:
- digestive system: burning sensation of the tongue, flatulence, pain and discomfort in the abdomen, attacks of hiccups, bruxism, dysphagia, sialorrhea (hypersalivation), heartburn, dyspepsia;
- metabolism: decrease / increase in body weight, edema;
- sense organs: oculogyric crises, taste disturbance, blurred vision, diplopia;
- respiratory system: cough, sore throat;
- nervous system: blepharospasm, peripheral neuropathy, gait instability, psychomotor agitation, euphoria, anxiety, insomnia, activation of latent Bernard-Horner syndrome, trismus, muscle cramps, increased hand tremor, numbness, ataxia, disorientation, decreased mental activity, asthenia, fainting, weakness;
- urinary system: urinary incontinence, urinary retention;
- others: priapism, malaise, hoarseness, malignant melanoma, flushing of the face, neck and chest;
- laboratory indicators: false positive reaction to ketone bodies in urine when using test strips to determine ketonuria (after boiling urine samples, this reaction does not change); also false negative results are possible when using the glucose oxidase method for determining glucosuria.
Overdose
The main symptoms: first, an increase, and then a decrease in blood pressure, anxiety, insomnia, anorexia, psychomotor agitation, confusion, heart rhythm disturbances, sinus tachycardia. Development of orthostatic hypotension is also possible. The symptoms of insomnia and anorexia can persist for several days.
Therapy: gastric lavage, the appointment of activated charcoal, symptomatic treatment (if necessary) in a hospital setting.
special instructions
Cancellation of Sindopa is carried out gradually, since a sudden cessation of its intake can serve the development of a symptom complex resembling a malignant neuroleptic syndrome (an increase in the activity of creatine phosphokinase in the blood serum, an increase in body temperature, muscle rigidity).
Patients who require a sudden decrease in the dose of the drug or discontinuation of its intake should be under medical supervision.
In elderly patients, the absorption of levodopa is higher than in young ones, which confirms the information about a decrease in the activity of DOPA-decarboxylase in tissues with age and with prolonged therapy with levodopa.
Epidemiological studies have shown that the risk of developing melanoma in patients with Parkinson's disease is higher than in the general population (approximately 2–6 times). It has not been established whether this increase is due to Parkinson's disease or to medications used to treat the disease. In this regard, it is important for patients and doctors who often and regularly use Sindopa according to indications to monitor the development of melanoma. Periodic skin examinations by qualified specialists (eg dermatologists) are recommended. In cases of long-term treatment, periodic monitoring of the hematopoietic system, cardiovascular system, kidney and liver function, monitoring of the patient's mental status is necessary.
If it is necessary to use general anesthesia during surgery, the dose of Sindopa is not reduced if the patient can take the drug and liquid inside. In cases of using cyclopropane and halothane, the drug is discontinued 8 hours (minimum) before surgery. After the operation, therapy is continued at usual doses.
In open-angle glaucoma, intraocular pressure is regularly monitored.
Influence on the ability to drive vehicles and complex mechanisms
During the period of admission to Sindopa, you should refrain from driving and conducting potentially hazardous activities.
Application during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Pediatric use
Sindopa is contraindicated in children under the age of 18.
With impaired renal function
Sindop is prescribed with caution to patients with severe renal impairment.
For violations of liver function
Sindop is prescribed with caution to patients with severe hepatic dysfunction.
Drug interactions
With the combined use of Sindopa with certain drugs / substances, the following effects may develop:
- tricyclic antidepressants: the bioavailability of levodopa decreases;
- D2-dopamine receptor blockers: the effect of the drug decreases;
- sympathomimetics: their effect may increase, which requires a decrease in their dose;
- amantadine: mutually potentiates the effect of levodopa;
- methyldopa: mutually potentiates the side effects of levodopa;
- pyridoxine: increases the peripheral metabolism of levodopa, so less of it penetrates the blood-brain barrier; if, when using such a combination, inhibitors of peripheral DOPA-decarboxylase are not additionally prescribed, the therapeutic effect of levodopa decreases;
- m-anticholinergics, reserpine, papaverine, thioxanthene derivatives, clonidine, phenytoin, diazepam: may reduce the antiparkinsonian effect of Sindopa;
- means for inhalation anesthesia, β-adrenomimetics: when combined with levodopa, the risk of developing cardiac arrhythmias may increase;
- tricyclic antidepressants: an increase in blood pressure and the development of dyskinesia are possible;
- antihypertensive drugs: postural hypotension is likely to develop, which requires special care during the period of combined therapy with Sindopa;
- MAO inhibitors: the risk of a hypertensive crisis (the combination is contraindicated).
Analogs
Analogs of Sindopa are: Tremonorm, Tidomet forte, Nakom, Madopar fast-acting tablets (dispersible) "125", Carbidopa / Levodopa, Duodopa.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 30 ° C. Keep out of the reach of children.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Sindop
According to reviews, Sindopa, with long-term therapy, significantly improves the condition of patients with Parkinson's disease.
Price for Sindopa in pharmacies
The approximate price of Sindopa tablets at a dosage of 250 + 25 (for 50 pieces in a package) is 140–192 rubles.
Sindopa: prices in online pharmacies
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Drug name Price Pharmacy |
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Sindopa 250 + 25 mg tablets 50 pcs. 183 r Buy |
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Sindopa tablets 250mg + 25mg 50 pcs. 188 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
